4-(2-amino-ethyl)-[1,3]dioxolan-2-one | 1268522-22-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机碳酸及其衍生物
• 英文名称: 4-(2-amino-ethyl)-[1,3]dioxolan-2-one
• 英文别名: 4-(2-aminoethyl)-[1,3]dioxolan-2-one；4-(2-aminoethyl)-1,3-dioxolan-2-one
• CAS: 1268522-22-0
• 化学式: C₅H₉NO₃
• mdl: MFCD18632757
• 分子量: 131.131
• InChiKey: ROEMPJJKJHRVET-UHFFFAOYSA-N

物化性质

• 沸点：
  310.5±15.0 °C(Predicted)
• 密度：
  1.208±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  61.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  在 palladium 10% on activated carbon 氢气 作用下， 以 甲醇 为溶剂， 以77%的产率得到4-(2-amino-ethyl)-[1,3]dioxolan-2-one
  参考文献：
  名称：

  [EN] HETEROCYCLIC AMIDES AS ROCK INHIBITORS
  [FR] AMIDES HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE ROCK

  摘要：

  公开号：

  WO2011107608A8

文献信息

• NOVEL ROCK INHIBITORS
  申请人：Leysen Dirk

  公开号：US20140057942A1

  公开（公告）日：2014-02-27

  The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, —NH—, or a direct bond; Y is —NH— or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of: Formula (II), Ar is selected from the group comprising: Formula (III), R 2 is hydrogen or methyl; R 8 is hydrogen, methyl, halogen, or alkynyl; R 1 is an aryl or heteroaryl more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

  本发明涉及新型激酶抑制剂，其化学式为(I)，其中X是氧、—NH—或直接键；Y是—NH—或直接键；n是从0到4的整数；m是从0到4的整数；Cy代表由饱和（多）环组成的二价基团，包括融合的、双的、螺环或桥接的碳环和杂环；特别是从以下组中选择：化学式（II），Ar是从包括化学式（III）的组中选择；R2是氢或甲基；R8是氢、甲基、卤素或炔基；R1是芳基或杂芳基，更具体地是ROCK抑制剂，包含此类抑制剂的组合物，特别是药品，以及此类抑制剂在治疗和预防疾病中的用途。特别是，本发明涉及新型ROCK抑制剂，包含此类抑制剂的组合物，特别是药品，以及此类抑制剂在治疗和预防疾病中的用途。此外，本发明还涉及治疗方法以及使用所述化合物在制造药品中的应用，用于治疗包括性功能障碍、炎症性疾病、眼科疾病和呼吸系统疾病等多种治疗适应症。
• HETEROCYCLIC AMIDES AS ROCK INHIBITORS
  申请人：Leysen Dirk

  公开号：US20120322801A1

  公开（公告）日：2012-12-20

  The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

  本发明涉及新的激酶抑制剂，更具体地说是ROCK抑制剂，包括这些抑制剂的组合物，特别是制药用途的组合物，并且涉及使用这些抑制剂在治疗和预防疾病方面的用途。特别是，本发明涉及新的ROCK抑制剂，包括这些抑制剂的组合物，特别是制药用途的组合物，并且涉及使用这些抑制剂在治疗和预防疾病方面的用途。此外，本发明还涉及治疗和使用所述化合物制造药物的方法，应用于多种治疗适应症，包括性功能障碍、炎症性疾病、眼科疾病和呼吸系统疾病。
• Rock inhibitors
  申请人：Leysen Dirk

  公开号：US09073905B2

  公开（公告）日：2015-07-07

  The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, —NH—, or a direct bond; Y is —NH— or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of: Formula (II), Ar is selected from the group comprising: Formula (III), R2 is hydrogen or methyl; R8 is hydrogen, methyl, halogen, or alkynyl; R1 is an aryl or heteroaryl more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

  本发明涉及公式（I）的新型激酶抑制剂，其中X为氧、—NH—或直接键；Y为—NH—或直接键；n为0至4的整数；m为0至4的整数；Cy代表由饱和（多）环组成的二价基团，包括融合的、双、螺旋或桥接的碳环和杂环；特别是从以下组中选出的：公式（II），其中Ar从包括的组中选出：公式（III），R2为氢或甲基；R8为氢、甲基、卤素或炔基；R1为芳香族或杂环族，更具体地为ROCK抑制剂，包括该类抑制剂的组合物，特别是制药用的组合物，以及该类抑制剂在治疗和预防疾病中的应用。特别地，本发明涉及新型ROCK抑制剂，包括该类抑制剂的组合物，特别是制药用的组合物，以及该类抑制剂在治疗和预防疾病中的应用。此外，本发明涉及使用所述化合物治疗和应用于制造药物的方法，用于多种治疗适应症，包括性功能障碍、炎症性疾病、眼科疾病和呼吸系统疾病。
• Heterocyclic amides as rock inhibitors
  申请人：Leysen Dirk

  公开号：US08815873B2

  公开（公告）日：2014-08-26

  The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

  本发明涉及新的激酶抑制剂，更具体地说是ROCK抑制剂，包括这些抑制剂的组合物，特别是制药组合物，以及在治疗和预防疾病方面使用这些抑制剂的用途。特别地，本发明涉及新的ROCK抑制剂，包括这些抑制剂的组合物，特别是制药组合物，以及在治疗和预防疾病方面使用这些抑制剂的用途。此外，本发明还涉及使用该化合物的治疗方法和用于制造药物的应用，适用于多种治疗适应症，包括性功能障碍、炎症性疾病、眼科疾病和呼吸系统疾病。
• [EN] NOVEL ROCK INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE ROCK
  申请人：AMAKEM NV

  公开号：WO2012146724A3

  公开（公告）日：2013-01-17